Quality Control of Methyl 3-(bromomethyl)benzoateIn 2017 ,《Stilbene Boronic Acids Form a Covalent Bond with Human Transthyretin and Inhibit Its Aggregation》 was published in Journal of Medicinal Chemistry. The article was written by Smith, Thomas P.; Windsor, Ian W.; Forest, Katrina T.; Raines, Ronald T.. The article contains the following contents:
Transthyretin (TTR) is a homotetrameric protein. Its dissociation into monomers leads to the formation of fibrils that underlie human amyloidogenic diseases. The binding of small mols. to the thyroxin-binding sites in TTR stabilizes the homotetramer and attenuates TTR amyloidosis. Herein, we report on boronic acid-substituted stilbenes that limit TTR amyloidosis in vitro. Assays of affinity for TTR and inhibition of its tendency to form fibrils were coupled with X-ray crystallog. anal. of nine TTR·ligand complexes. The ensuing structure-function data led to a sym. diboronic acid that forms a boronic ester reversibly with serine 117. This diboronic acid inhibits fibril formation by both wild-type TTR and a common disease-related variant, V30M TTR, as effectively as does tafamidis, a small-mol. drug used to treat TTR-related amyloidosis in the clinic. These findings establish a new modality for covalent inhibition of fibril formation and illuminate a path for future optimization. In the part of experimental materials, we found many familiar compounds, such as Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8Quality Control of Methyl 3-(bromomethyl)benzoate)
Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8) belongs to organobromine compounds.Depending on the type of carbon to which the bromine is bonded, organic bromide could be alkyl, alkenyl, alkynyl, or aryl. Quality Control of Methyl 3-(bromomethyl)benzoate Due to the reactivity of bromide, they are used as potential precursors or important intermediates in organic synthesis.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary